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2,6-Difluorobenzamide inhibitors of the bacterial cell division protein FtsZ: design, synthesis and Structure Activity Relationship study.

著者 Straniero V , Valoti E , Zanotto C , Straniero L , Casiraghi A , Duga S , Radaelli A , de Giuli Morghen C
ChemMedChem.2017 Jun 06 ; ():.
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A wide variety of drug-resistant microorganism are continuously emerging, restricting the therapy of common bacterial infections. Originally potent antimicrobial agents are now no longer helpful, due to their weak or null activity towards these antibiotic-resistant bacteria. In addition, none of the recently approved antibiotics affects innovative targets, resulting in a requirement of novel drugs, with innovative antibacterial mechanisms of action. The essential cell division protein FtsZ (Filamentous temperature sensitive Z) emerged as a possible target, thanks to its ubiquitous expression and its homology to eukaryotic -tubulin. In the latest years, several compounds proved to interact with this prokaryotic protein and to selectively inhibit bacterial cell division. Recently, our research group developed interesting derivatives displaying good antibacterial activities against methicillin-resistant Staphylococcus aureus, as well as vancomycin-resistant Enterococcus faecalis and Mycobacterium tuberculosis. The aim of the present work is to summarize the Structure Activity Relationship of differently substituted heterocycles, linked by a methylenoxy-bridge to the 2,6-difluoro-benzamide, and to validate FtsZ as the real target of this class of antimicrobicals.
PMID: 28586174 [PubMed - as supplied by publisher]
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